Design,synthesis and biological evaluation of LpxC inhibitors with novel hydrophilic terminus |
| |
| Authors: | Shi Ding Wen-Ke Wang Qiao Cao Wen-Jing Chu Le-Fu Lan Wen-Hao Hu Yu-She Yang |
| |
| Affiliation: | a State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China;b Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, East China Normal University, Shanghai 200062, China |
| |
| Abstract: | ![]()
In order to develop novel LpxC inhibitors with good activities and metabolic stability, two series of compounds with hydrophilic terminus have been synthesized and their in vitro antibacterial activities against Escherichial coli and Pseudomonas aeruginosa were evaluated. Especially, compounds 22b and c exhibited comparable antibacterial activities to CHIR-090 and better metabolic stability than CHIR-090 and LPC-011 in liver microsomes (rat andmouse), which indicated the terminal methylsulfone may be a preferred structure in the design of LpxC inhibitors and worthy of further investigations. |
| |
| Keywords: | LpxC CHIR-090 Kojic acid derivatives Methylsulfone derivatives Metabolic stability |
| 本文献已被 CNKI 等数据库收录！ |
| 点击此处可从《中国化学快报》浏览原始摘要信息 |
|
点击此处可从《中国化学快报》下载全文 |
|
